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Transcript
TRINITY COLLEGE DUBLIN
Trinity Research & Innovation-Licensing Opportunity
AN EFFICIENT CATALYST
A novel catalyst for the production of enantiomer specific pregabalin.
Technology Overview
Progablin is a blockbuster anticonvulsat drug, marketed as Lyrica, used to treat neuralgiac pain. A difficulty in its
synthesis is ensuring that the right chiral enantiomer is formed. Trinity researchers have developed a new method
to selectively synthesise the appropriate enatiomer of an immediate precursor to the drug using a highly efficient
catalyst. The product yields and ‘enantio-selectiveness’ of the new process are uniformly excellent and the catalyst
can be used under very mild and scalable conditions.
Advantages:
Development Stage:
The synthesis of ‘enantiopure’ pregabalin has the
requirement for a step which discards 50% of the
product which is inefficient and wasteful. The
technology on offer here modifies the synthesis
process to preferentially create the desired
enantiomer.
The catalyst has been reduced to practice and the
efficiency of its enantiomer selectiveness is known.
This invention is based on a desymmetrisation step –
a meso starting material is converted to a chiral
enantioenriched product in a highly selective
manner. Thus the need for a costly resolution step
has been removed.
A patent application has been filed in Europe
Other similar attempts to create a enanatiomer
sensitive catalyst have proved impractical due to a
requirement for large amounts of catalyst (quinine
or quinidine) and the need for low reaction
temperatures (50 and -78 °C).
The catalyst presented here is efficient to the point
where it can be used at low levels of 1-2 mol%.
In addition this catalyst functions at ambient
temperatures (or lower, if required).
Principal Inventor(s):
Dr. Stephen Connon, Aldo Peschiulli, Lyn Markey
Patent:
TCD Ref: SC01-181-01
Contact:
Name: Graham McMullin, Ph.D
Position: Technology Transfer Case Manager
Tel: + 353 1 896-1711
Email: [email protected]